TRPA1 modulation by Sigma-1 receptor prevents oxaliplatin-induced painful peripheral neuropathy
By Aida Marcotti, Jorge Fernández-Trillo, Alejandro González, Marta Vizcaíno-Escoto, Pablo Ros-Arlanzón, Luz Romero, José Miguel Vela, Ana Gomis, Félix Viana, and Elvira de la Peña Excerpt from the article published in Brain, Volume 146, Issue 2, February 2023, Pages 475–491, DOI: https://doi.org/10.1093/brain/awac273 Editor’s Highlights Abstract Chemotherapy-induced peripheral neuropathy is a frequent, disabling side effect of anticancer […]
Continue ReadingαN-Acetyl β-Endorphin Is an Endogenous Ligand of σ1Rs That Regulates Mu-Opioid Receptor Signaling by Exchanging G Proteins for σ2Rs in σ1R Oligomers
By Javier Garzón-Niño, Elsa Cortés-Montero, María Rodríguez-Muñoz, and Pilar Sánchez-Blázquez Excerpt from the article published in the International Journal of Molecular Sciences. 2023; 24(1):582, 29 December 2022, DOI: https://doi.org/10.3390/ijms24010582 Editor’s Highlights Abstract The opioid peptide β-endorphin coexists in the pituitary and brain in its αN-acetylated form, which does not bind to opioid receptors. We now report […]
Continue ReadingHevin/Sparcl1 drives pathological pain through spinal cord astrocyte and NMDA receptor signaling
By Gang Chen, Jing Xu, Hao Luo, Xin Luo, Sandeep K. Singh, Juan J. Ramirez, Michael L. James, Joseph P. Mathew, Miles Berger, Cagla Eroglu, and Ru-Rong Ji Excerpt from the article published in JCI Insight, Volume 7, Issue 23 on December 8, 2022, e161028. DOI: https://doi.org/10.1172/jci.insight.161028. Editor’s Highlights Abstract High endothelial venule protein/SPARC-like 1 […]
Continue ReadingThe sigma-1 receptor curtails endogenous opioid analgesia during sensitization of TRPV1 nociceptors
By M. Carmen Ruiz-Cantero, Elsa Cortés-Montero, Aakanksha Jain, Ángeles Montilla-García, Inmaculada Bravo-Caparrós, Jaehoon Shim, Pilar Sánchez-Blázquez, Clifford J. Woolf, José M. Baeyens, and Enrique J. Cobos Excerpt from the article published in British Journal of Pharmacology, 1– 20, 07 December 2022, DOI: https://doi.org/10.1111/bph.16003 Editor’s Highlights Abstract Background and Purpose: Peripheral sensitization contributes to pathological pain. While prostaglandin […]
Continue ReadingSigma Antagonists for Treatment of Neuropathic Pain Syndromes in Cancer Patients: A Narrative Review
By Joseph V. Pergolizzi, Jr. and Jo Ann LeQuang Article published in Journal of Cancer Research Updates, 11, 70–77, 2022-10-27, DOI: https://doi.org/10.30683/1929-2279.2022.11.10 Abstract Almost 40% of cancer patients have neuropathic pain or mixed pain with a neuropathic component, which can be intense, debilitating, and challenging to treat. New studies on sigma receptors show these enigmatic ligand-binding […]
Continue ReadingBispecific sigma-1 receptor antagonism and mu-opioid receptor partial agonism: WLB-73502, an analgesic with improved efficacy and safety profile compared to strong opioids
By Alba Vidal-Torres, Begoña Fernández-Pastor, Mónica García, Eva Ayet, Anna Cabot, Javier Burgueño, Xavier Monroy, Bertrand Aubel, Xavier Codony, Luz Romero, Rosalía Pascual, Maria Teresa Serafini, Gregorio Encina, Carmen Almansa, Daniel Zamanillo, Manuel Merlos, and José Miguel Vela Excerpt from the article published in Acta Pharmaceutica Sinica B, September 25, 2022, ISSN 2211-3835, DOI: https://doi.org/10.1016/j.apsb.2022.09.018 […]
Continue ReadingCharacterization of CM-398, a Novel Selective Sigma-2 Receptor Ligand, as a Potential Therapeutic for Neuropathic Pain
By Lisa L. Wilson, Amy R. Alleyne, Shainnel O. Eans, Thomas J. Cirino, Heather M. Stacy, Marco Mottinelli, Sebastiano Intagliata, Christopher R. McCurdy, and Jay P. McLaughlin Excerpt from the article published in Molecules 2022, 27(11), 3617; DOI: https://doi.org/10.3390/molecules27113617 Editor’s Highlights First identified as Tmem97, the sigma-2 receptor (S2R) was only recently cloned in 2017 and is known […]
Continue ReadingPharmacologic Management of Persistent Pain in Cancer Survivors
by Glare, P., Aubrey, K., Gulati, A. et al. Excerpt from the article published in Drugs (2022). https://doi.org/10.1007/s40265-022-01675-6 Editor’s Highlights Abstract Improvements in screening, diagnosis and treatment of cancer has seen cancer mortality substantially diminish in the past three decades. It is estimated there are almost 20 million cancer survivors in the USA alone, but some 40% […]
Continue ReadingSigma-1 receptor increases intracellular calcium in cultured astrocytes and contributes to mechanical allodynia in a model of neuropathic pain
By Jae-Gyun Choi, Sheu-Ran Choi, Dong-Wook Kang, Jaehyuk Kima, Jin Bong Park, Jang-Hern Lee, and Hyun-Woo Kim Introduction to the article published in Brain Research Bulletin, Volume 178, January 2022, Pages 69-81 DOI: https://doi.org/10.1016/j.brainresbull.2021.11.010 Autors’ Highlights Abstract Recent studies have revealed that glial sigma-1 receptor (Sig-1R) in the spinal cord may be a critical factor […]
Continue ReadingSigma-1 receptors and progesterone metabolizing enzymes in nociceptive sensory neurons of the female rat trigeminal ganglia: A neural substrate for the antinociceptive actions of progesterone
By Rebecca S. Hornung, Namrata GR Raut, Daisy J. Cantu, Lauren M Lockhart, and Dayna L. Averitt Excerpt from the article published in Molecular Pain. January 2022. DOI: 10.1177/17448069211069255 Editor’s Highlights Pain signaled by the trigeminal nociceptors is common, often debilitating, and includes musculoskeletal, neurovascular, and neuropathic pain Trigeminal sensory neurons are an anatomical substrate for the […]
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